Application of tri(hydroxymethyl)aminomethane hydrochloride solution in medicine for treating hyperuricemia

A tris, hyperuricemia technology, applied in the field of pharmaceutical applications, can solve the problem of no tris hydrochloride solution, etc., to achieve the effect of increasing water solubility

Pending Publication Date: 2020-12-01
BEIJING CHANGSHENG PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0034] Also there is no tris hydrochloride solution at present, (tromethamine hydrochloride...

Method used

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  • Application of tri(hydroxymethyl)aminomethane hydrochloride solution in medicine for treating hyperuricemia
  • Application of tri(hydroxymethyl)aminomethane hydrochloride solution in medicine for treating hyperuricemia
  • Application of tri(hydroxymethyl)aminomethane hydrochloride solution in medicine for treating hyperuricemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0145] Tris and uric acid combined reaction to form "uric acid·TRIs conjugate" and preliminary research experiments on "uric acid·TRIs conjugate":

[0146] 1. Synthesis

[0147] Weigh 300 mg of uric acid, add it to 100 ml of 0.6mol / L (PH7.4) tris hydrochloride solution, stir for 10 minutes, the uric acid is completely dissolved, the solution becomes clear, continue to stir, and then a milky flocculent precipitate is formed , Vacuum filtration and drying to obtain 480 mg of white blocky uric acid·trishydroxymethylaminomethane conjugate.

[0148] 2. Solubility

[0149] ① Take 56mg of white blocky uric acid·trishydroxymethylaminomethane conjugate and add it to 100ml of water, stir for 1 hour, the white block is completely dissolved, the solution is clear and no longer crystallized. However, continuing to add uric acid-trishydroxymethylaminomethane conjugates in this solution will make the solution supersaturated and make part of the conjugates insoluble.

[0150] It shows that...

Embodiment 2

[0157] Imitating the concentration of the drug in the blood after the drug is used in the human body, the test of dissolving uric acid crystals in water

[0158] Test material: 1, uric acid (crystal), 2, Tris hydrochloride solution (PH7.4 ± 0.5) 0.3mol / L or 0.6mol / L solution (new medicine of the present invention), 3, water for injection.

[0159] Experimental Design: In Vitro Simulation Test

[0160] Assuming a 60 kg heavy hyperuric acid patient, its total blood 4500ml, 7mg uric acid is dissolved in 100ml blood; 3mg uric acid crystals are arranged, now use new drug trishydrochloride hydrochloride solution of the present invention (PH7.4 ± 0.5) 0.3mol / L or 0.6mol / L solution treatment, the dosage is 0.5ml / kg-3ml / kg for one administration.

[0161] 1. Assuming that the total blood volume of a 60 kg patient is 4500ml, 7mg of uric acid is dissolved in 100ml of blood;

[0162] Corresponding test: Take 10mg of uric acid + 100ml of water + 0.66ml, 0.3mol / L liquid medicine, put it i...

Embodiment 3

[0181] Dissolution test of sodium urate crystal in medicinal liquid of the present invention

[0182] 1. Take 0.3 mol / L tris hydrochloride solution (PH7.4±0.5), 35 ml, add 50 mg of sodium urate, put it in a shaker at 36.5 °C for 60 rpm, keep warm and shake for 4 hours, solid particles Completely dissolved, the solution was clear.

[0183] 2. Take 35 ml of purified water, add 50 mg of sodium urate, put it in a shaker at 36.5°C for 60 rpm, keep it warm and shake for 4 hours, most of the solid particles are not dissolved, and the solution is very turbid.

[0184] Test result: illustrate that medicinal liquid of the present invention can dissolve sodium urate crystal.

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Abstract

The invention discloses application of a salt formed by combining tri(hydroxymethyl)aminomethane and acid radicals or an aqueous solution of the salt to preparing of a medicine for treating hyperuricemia, gout, acute and chronic arthritis, urinary calculus diseases and related diseases. The treatment action mechanism is as follows: tri(hydroxymethyl)aminomethane and uric acid are combined throughhydrogen bonds to generate a uric acid-tri(hydroxymethyl)aminomethane conjugate, uric acid crystallization is prevented, and uric acid crystals (calculi) are dissolved; meanwhile, the combination of uric acid with macromolecular substances such as blood fat and blood sugar is reduced, and the influence of uric acid on blood fat and blood sugar is reduced. Compared with existing three action mechanisms of 1, intake reduction, 2, endogenous synthesis inhibition and 3, kidney excretion promotion for treating hyperuricemia, the action mechanism of the invention can be called as a fourth action mechanism. The invention can also be referred to as a fourth treatment method for hyperuricemia. And the problems of uric acid crystallization and influence of uric acid on blood fat and blood sugar aresolved in a targeted manner. The action mechanism is clear; the curative effect is good; and the side effect is small.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical applications, and relates to a combination of trishydroxymethylaminomethane and an inorganic acid or an organic acid, or an aqueous solution of the combination for the treatment of hyperuricemia, gout, acute and chronic arthritis, and urinary calculi. The application and mechanism of action in drugs for diseases and related diseases. In particular, it relates to the application of Tris hydrochloride solution (PH7.4±0.5) as a medicine for treating hyperuricemia, gout, arthritis, urinary calculi and related diseases. Background technique: [0002] Uric acid, this substance, makes many patients with hyperuricemia complain and hate. It seems to be a substance that everyone shouts to get rid of. [0003] In fact, what many people don't know is that uric acid is the "hero" for our human beings to evolve from apes. [0004] Current research believes that humans have experienced multiple related gene mut...

Claims

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Application Information

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IPC IPC(8): A61K31/205A61P19/06A61P19/02A61P13/04A61P13/12
CPCA61K31/205A61P13/04A61P13/12A61P19/02A61P19/06
Inventor 不公告发明人
Owner BEIJING CHANGSHENG PHARM TECH CO LTD
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